Theacrine Explained

Theacrine, also known as 1,3,7,9-tetramethyluric acid, is a purine alkaloid found in Cupuaçu (Theobroma grandiflorum) and in a Chinese tea known as kucha (Camellia assamica var. Kucha).[1] [2] It shows anti-inflammatory and analgesic effects and appears to affect adenosine signalling in a manner similar to caffeine.[3] In kucha leaves, theacrine is synthesized from caffeine in what is thought to be a three-step pathway. Theacrine and caffeine are structurally similar.

Pharmacology

Pharmacodynamics

The exact mechanism of action of theacrine is uncertain, as no binding affinities have been published. However, animal research involving selective A1 and A2A adenosine agonists found theacrine pretreatment attenuated the expected motor depression induced by adenosine agonism, indicating that theacrine is likely an adenosine antagonist.[2]

Administration of selective dopamine D1 and D2 antagonists demonstrate that, similarly to caffeine,[4] theacrine's actions are in part mediated by dopamine receptors. This should not be taken as evidence that theacrine directly interacts with and/or augments dopamine receptors distinct from caffeine, as some marketers have misleadingly claimed.

Pharmacokinetics

Theacrine has half-life of 30 to 33 hours.[5]

Safety

Theacrine has demonstrated clinical safety and non-habituating effects in healthy humans over eight weeks of daily use at up to 300 mg/day.[6] Moreover, there was no evidence of the tachyphylaxis typical of neuroactive agents like caffeine and other stimulants.[6]

In animal studies, theacrine has an LD50 of 810 mg/kg,[3] [6] compared to 265 mg/kg for caffeine.[7]

See also

Notes and References

  1. 12009315. 2002. Zheng. XQ. Ye. CX. Kato. M. Crozier. A. Ashihara. H. Theacrine (1,3,7,9-tetramethyluric acid) synthesis in leaves of a Chinese tea, kucha (Camellia assamica var. Kucha). 60. 2. 129–34. Phytochemistry. 10.1016/s0031-9422(02)00086-9. 2002PChem..60..129Z .
  2. 10.1016/j.pbb.2012.04.014. Locomotor activation by theacrine, a purine alkaloid structurally similar to caffeine: Involvement of adenosine and dopamine receptors. 2012. Feduccia. Allison A.. Wang. Yuanyuan. Simms. Jeffrey A.. Yi. Henry Y.. Li. Rui. Bjeldanes. Leonard. Ye. Chuangxing. Bartlett. Selena E.. Pharmacology Biochemistry and Behavior. 102. 2. 241–248. 22579816. 31549989.
  3. 10.1016/j.fitote.2010.03.008. Theacrine, a purine alkaloid with anti-inflammatory and analgesic activities. 2010. Wang. Yuanyuan. Yang. Xiaorong. Zheng. Xinqiang. Li. Jing. Ye. Chuangxing. Song. Xiaohong. Fitoterapia. 81. 6. 627–631. 20227468.
  4. Garrett . B. E. . Holtzman . S. G. . January 1994 . D1 and D2 dopamine receptor antagonists block caffeine-induced stimulation of locomotor activity in rats . Pharmacology, Biochemistry, and Behavior . 47 . 1 . 89–94 . 10.1016/0091-3057(94)90115-5 . 0091-3057 . 7906891. 23508010 .
  5. Caffeine and Methylliberine: A Human Pharmacokinetic Interaction Study . Mondal . Goutam . Wang . Yan-Hong . 2021-01-06 . Pharmacology and Therapeutics . 10.1101/2021.01.05.21249234 . en . Butawan . Matthew . Bloomer . Richard J . Yates . Ryan.
  6. Taylor L, Mumford P, Roberts M, Hayward S, Mullins J, Urbina S, Wilborn C . Safety of TeaCrine®, a non-habituating, naturally-occurring purine alkaloid over eight weeks of continuous use . Journal of the International Society of Sports Nutrition . 13 . 2 . 2016 . 26766930 . 4711067 . 10.1186/s12970-016-0113-3 . free .
  7. Warszawski D, Gorodischer R, Kaplanski J . Comparative toxicity of caffeine and aminophylline (theophylline ethylenediamine) in young and adult rats . Biology of the Neonate . 34 . 1–2 . 68–71 . 1978 . 698326 . 10.1159/000241107.

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Theacrine".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.